With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC50 values of 4.09 and 5.11 µM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.

中文翻译：

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无毒芳基吡咯基查尔酮衍生物的合成、结构和体外抗锥虫活性


为了鉴定具有抗原虫活性的查耳酮衍生物，以中等至良好的产率合成了一组相对未开发的基于芳基吡咯的查耳酮衍生物。在体外评估所得化合物针对培养的布氏锥虫 427 菌株的潜在活性。几种化合物大多表现出适度的体外抗锥虫活性，其中化合物 10e 和 10h 成为活性候选物，IC50 值分别为 4.09 和 5.11 µM。更重要的是，对它们针对人宫颈腺癌 (HeLa) 细胞系的活性进行的同时评估表明，这些化合物是无毒的。